R8781

Rapamycin

Ready Made Solution, 2.5 mg/mL in DMSO (2.74 mM), from Streptomyces hygroscopicus

• Synonym(s): 23,27-Epoxy-3H-pyrido[2,1-c][1,4]oxaazacyclohentriacontine solution
• Empirical Formula (Hill Notation): C₅₁H₇₉NO₁₃
• Molecular Weight: 914.17
• EC Number: 200-664-3
• NACRES: NA.77

Properties

• Quality Level: 300
• biological source: Streptomyces hygroscopicus
• vapor pressure: 0.56 hPa ( 20 °C)
• sterility: 0.2 μm filtered
• assay: ≥95% (HPLC)
• form: solution
• autoignition temp.: 301 °C
• concentration: 2.5 mg/mL in DMSO (2.74 mM)
• color: colorless to yellow
• antibiotic activity spectrum: fungi; yeast
• Mode of action: enzyme | inhibits
• originator: Pfizer
• storage temp.: −20°C

Description

Biochem/physiol Actions

Rapamycin is a macrocyclic triene antibiotic possessing potent immunosuppressant and anticancer activity. It forms a complex with FKBP12 that binds to and inhibits the molecular target of rapamycin (mTOR). mTOR is a member of the phosphoinositide kinase-related kinase (PIKK) family that enhances cellular proliferation via the phosphoinositol 3-kinase/Akt signaling pathway. Inhibition of this pathway by rapamycin blocks downstream elements that result in cell cycle arrest in G1. The effectors of mTOR action include 4EBP1 and S6K1.

Features and Benefits

This compound is featured on the Phosphoinositide Kinases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Pfizer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Packaging

200uL

Other Notes

Keep container tightly closed in a dry and well-ventilated place. Store under inert gas. Is Hygroscopic.
Rapamycin has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the Rapamycin probe summary on the Chemical Probes Portal website.

Safety Information

• Storage Class Code: 10 - Combustible liquids
• WGK: WGK 1
• Flash Point(F): 188.6 °F - closed cup
• Flash Point(C): 87 °C - closed cup
• Personal Protective Equipment: dust mask type N95 (US), Eyeshields, Gloves